The efficacy of protracted schedules of therapy of the topoisomerase I inhibitors 9-dimethylaminomethyl-10-hydroxycamptothecin
(topotecan) and 7-ethyl-10-[4-(1-piperidino)-1-…

The poor prognosis for patients with aggressive or metastatic tumors and the toxic side
effects of currently available treatments necessitate the development of more effective tumor-…

Carboxylesterases (CE) are ubiquitous enzymes responsible for the metabolism of xenobiotics.
Because the structural and amino acid homology among esterases of different classes, …

Human carboxylesterase 1 (hCE1) is a broad-spectrum bioscavenger that plays important
roles in narcotic metabolism, clinical prodrug activation, and the processing of fatty acid and …

Mammalian carboxylesterases cleave the anticancer prodrug CPT-11 (Irinotecan) into SN-38,
a potent topoisomerase I poison, and 4-piperidino-piperidine (4PP). We present the 2.5 Å …

Irinotecan[7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin(CPT-11)] is
metabolized by esterases to yield the potent topoisomerase I poison 7-ethyl-10-…

Background The p53 tumor suppressor gene is the most commonly mutated gene in human
cancer, and mutations arise in a wide variety of tumor types. Wild‐type p53 functions as a …

Neural stem cells and progenitor cells migrate selectively to tumor loci in vivo. We exploited
the tumor-tropic properties of HB1.F3.C1 cells, an immortalized cell line derived from human …

Nuclear extracts from teniposide (VM-26)-resistant sublines of the human leukemic cell line
CCRF-CEM have decreased levels of DNA topoisomerase II catalytic activity and decreased …

Background Patients diagnosed with metastatic cancer have almost uniformly poor prognoses.
The treatments available for patients with disseminated disease are usually not curative …